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品質等級
化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
H2O: 2 mg/mL, clear
儲存溫度
2-8°C
InChI
1S/C15H18FN3O2S/c1-11-8-17-6-3-7-19(11)22(20,21)14-5-2-4-12-9-18-10-13(16)15(12)14/h2,4-5,9-11,17H,3,6-8H2,1H3/t11-/m0/s1
InChI 密鑰
QSKQVZWVLOIIEV-NSHDSACASA-N
生化／生理作用
Ripasudil (K-115) is a more potent and selective rho-associated protein kinase (ROCK) inhibitor (IC50 = 51 nM/ROCK1, 19 nM/ROCK2, 2.1 μM/PKACα, 27 μM/PKC, and 0.37 μM/CaMKII?) than Y-27632 and HA-1077 (Fasudil). Ripasudil demonstrates in vivo efficacy in reducing intraocular pressure (IOP) by stimulating aqueous humour drainage through the trabecular meshwork.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Yoshio Kaneko et al.
Scientific reports, 6, 19640-19640 (2016-01-20)
Ripasudil hydrochloride hydrate (K-115), a specific Rho-associated coiled-coil containing protein kinase (ROCK) inhibitor, was the first ophthalmic solution developed for the treatment of glaucoma and ocular hypertension in Japan. Topical administration of K-115 decreased intraocular pressure (IOP) and increased outflow
Kotaro Yamamoto et al.
Investigative ophthalmology & visual science, 55(11), 7126-7136 (2014-10-04)
To investigate the effect of K-115, a novel Rho kinase (ROCK) inhibitor, on retinal ganglion cell (RGC) survival in an optic nerve crush (NC) model. Additionally, to determine the details of the mechanism of K-115's neuroprotective effect in vivo and
Seigo Nakabayashi et al.
Experimental eye research, 139, 132-135 (2015-07-22)
Ripasudil (K-115) is a novel Rho kinase inhibitor with a potent intraocular pressure-lowering effect. However, it is unclear whether ripasudil affects the retinal blood flow (RBF). We investigated the effect of ripasudil on feline retinal microcirculation. Ripasudil (5 μM, 50 μM or
Karly P Garnock-Jones
Drugs, 74(18), 2211-2215 (2014-11-22)
Ripasudil hydrochloride hydrate (Glanatec® ophthalmic solution 0.4 %; hereafter referred to as ripasudil) is a small-molecule, Rho-associated kinase inhibitor developed by Kowa Company, Ltd. for the treatment of glaucoma and ocular hypertension. This compound, which was originally discovered by D.
Tomoyuki Isobe et al.
Xenobiotica; the fate of foreign compounds in biological systems, 46(7), 579-590 (2015-12-19)
1. We examined the metabolism of ripasudil (K-115), a selective and potent Rho-associated coiled coil-containing protein kinase (ROCK) inhibitor, by in vitro and in vivo studies. 2. First, we identified metabolites and metabolic enzymes involved in ripasudil metabolism. Species differences were observed
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